Peptide exhibiting antibacterial and anti-inflammatory activities and method for treating medical condition with the same

Abstract

A peptide exhibiting both antibacterial and anti-inflammatory activities or a derivative thereof, including one of the following sequences: an amino acid sequence of SEQ ID NO: 1 or a variant thereof, and an amino acid sequence of SEQ ID NO: 2 or a variant thereof. The peptides synthesized in this disclosure exhibit antibacterial and anti-inflammatory effects, inhibiting one or more of the following: Escherichia coli, Staphylococcus aureus, Propionibacterium acnes, Candida albicans , as well as the expression of IL-6, IL-1B, CCL-2, IL-1, and NO.

What is claimed is: 
     
         1 . A peptide or a derivative thereof, comprising one of the following sequences:
 an amino acid sequence of SEQ ID NO: 1, or a variant thereof; and   an amino acid sequence of SEQ ID NO: 2, or a variant thereof.   
     
     
         2 . The peptide or a derivative thereof according to  claim 1 , wherein the variant of SEQ ID NO: 1 has ≥88% sequence identity with SEQ ID NO: 1, and the variant of SEQ ID NO: 2 has ≥88% sequence identity with SEQ ID NO: 2. 
     
     
         3 . The peptide or a derivative thereof according to  claim 1 , wherein the variant of SEQ ID NO: 1 has an amino acid sequence of SEQ ID NO: 3 or SEQ ID NO: 4. 
     
     
         4 . The peptide or a derivative thereof according to  claim 1 , wherein variation(s) in SEQ ID NO: 1 consists only of one or more conservative amino acid substitutions among amino acids within each of the following groups: (a) glycine, alanine, valine, leucine, and isoleucine; (b) phenylalanine, tyrosine, and tryptophan; (c) serine and threonine; (d) aspartate and glutamate; (e) glutamine and asparagine; and (f) lysine, arginine and histidine. 
     
     
         5 . The peptide or a derivative thereof according to  claim 1 , wherein each of the amino acid sequences of SEQ ID NO: 1 and SEQ ID NO: 2 comprises an N-terminal; a hydrogen atom of the N-terminal is substituted by CH 3 CH(OH)CO— or R 1 —CO—, and R 1  is selected from a group consisting of H, hydroxyl, amino, an alkyl group, and an alkenyl group. 
     
     
         6 . The peptide or a derivative thereof according to  claim 1 , wherein each of the amino acid sequences of SEQ ID NO: 1 and SEQ ID NO: 2 comprises a C-terminal; a hydrogen atom of the C-terminal is substituted by —NR 2 R 3  or —OR 2 , and R 2  and R 3  are independently selected from a group consisting of H, hydroxyl, amino, an alkyl group, and an alkenyl group. 
     
     
         7 . The peptide or a derivative thereof according to  claim 5 , wherein the alkyl group is selected from a group consisting of methyl, ethyl, isopropyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl, octyl, decyl, 2-ethylhexyl, 2-methylbutyl, and 5-methylhexyl. 
     
     
         8 . The peptide or a derivative thereof according to  claim 6 , wherein the alkyl group is selected from a group consisting of methyl, ethyl, isopropyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl, octyl, decyl, 2-ethylhexyl, 2-methylbutyl, and 5-methylhexyl. 
     
     
         9 . The peptide or a derivative thereof according to  claim 5 , wherein the alkenyl group is selected from a group consisting of vinyl, linoleyl, and oleyl. 
     
     
         10 . The peptide or a derivative thereof according to  claim 6 , wherein the alkenyl group is selected from a group consisting of vinyl, linoleyl, and oleyl. 
     
     
         11 . A pharmaceutical composition, comprising:
 a medication container; and   a therapeutically effective amount of the peptide or a derivative thereof of  claim 1 .   
     
     
         12 . The pharmaceutical composition of  claim 11 , wherein the peptide or a derivative thereof is in solid powder form in an amount of 200-2,500 mg per dose. 
     
     
         13 . The pharmaceutical composition of  claim 11 , further comprising an aqueous solution contained in the medication container; wherein the peptide or a derivative thereof is dissolved in the aqueous solution at a concentration of 3-30 mg/mL. 
     
     
         14 . A method for treating a medical condition in a patient, comprising administering to the patient a therapeutically effective amount of the peptide or a derivative thereof of  claim 1 . 
     
     
         15 . The method of  claim 14 , wherein an amount of the peptide or a derivative thereof is administered as a single dose is 200-2,500 mg per dose or 2-60 mg/kg of body weight. 
     
     
         16 . The method of  claim 14 , wherein the medical condition is acne and the peptide or a derivative thereof is administered topically to a treatment area on the patient's skin. 
     
     
         17 . A method for preparing a cosmetically or pharmaceutically acceptable salt comprising applying the peptide or a derivative thereof of  claim 1 . 
     
     
         18 . The method of  claim 17 , wherein the salt is formed by the peptide or a derivative thereof of  claim 1  with an organic base, and the organic base is ethylamine, diethylamine, arginine, lysine, histidine or piperazine. 
     
     
         19 . The method of  claim 17 , wherein the salt is formed by the peptide or a derivative thereof of  claim 1  with an inorganic acid or an organic acid; the organic acid is acetic acid, citric acid, malonic acid, maleic acid, tartaric acid, fumaric acid, benzoic acid, succinic acid, oxalic acid, or gluconic acid; and the inorganic acid is hydrochloric acid, sulphuric acid, boric acid or carbonic acid.